Pitavastatin

From Wikipedia, the free encyclopedia

Pitavastatin
Systematic (IUPAC) name
(E)-7-[2-cyclopropyl-4-(4-fluorophenyl) quinolin-3-yl]-3,5-dihydroxy-hept-6-enoic acid
Identifiers
CAS number	147511-69-1
ATC code	C10AA08
PubChem	6366718
Chemical data
Formula	C25H24FNO4
Mol. mass	421.461
Pharmacokinetic data
Bioavailability	60%
Protein binding	96%
Metabolism	hepatic
Half life	11 hours
Excretion	biliary
Therapeutic considerations
Pregnancy cat.	X
Legal status	prescription
Routes	oral tablets 1 & 2 mg

Pitavastatin (usually as a calcium salt) is a novel member of the medication class of statins.^[1] Like the other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis. It has been available in Japan since 2003, and is being marketed under licence in South Korea and in India.^[2] It is likely that pitavastatin will be approved for use in hypercholesterolaemia (elevated levels of cholesterol in the blood) and for the prevention of cardiovascular disease outside South and Southeast Asia as well.^[3]

Contents 1 Uses 2 Side-effects 3 Metabolism and interactions 4 History 5 References 6 External links

[edit] Uses

Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease.

[edit] Side-effects

Common statin-related side-effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins.^[3]

[edit] Metabolism and interactions

Most statins are metabolised in part by one or more hepatic cytochrome P450 enzymes, leading to an increased potential for drug interactions and problems with certain foods (such as grapefruit juice). Pitavastatin appears to be a substrate of CYP2C9, and not CYP3A4 (which is a common source of interactions in other statins).^[3]

[edit] History

Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) was discovered in Japan by Nissan Chemical Industries, Ltd. and developed further by Kowa Pharmaceuticals, Tokyo.^[3]

[edit] References

1. ^ Kajinami K, Takekoshi N, Saito Y. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev 2003;21:199-215. PMID 12931254.
2. ^ Zydus Cadila launches pitavastatin in India
3. ^ ^{a b c d} Mukhtar RY, Reid J, Reckless JP. Pitavastatin. Int J Clin Pract 2005;59:239-52. PMID 15854203.

[edit] External links

v • d • e Lipid modifying agents (C10) Statins Atorvastatin • Cerivastatin‡ • Fluvastatin • Lovastatin • Mevastatin • Pitavastatin • Pravastatin • Rosuvastatin • Simvastatin Fibrates Clofibrate‡ • Bezafibrate • Aluminium clofibrate • Gemfibrozil • Fenofibrate • Simfibrate • Ronifibrate • Ciprofibrate • Etofibrate • Clofibride Bile acid sequestrants Colestyramine • Colestipol • Colextran • Colesevelam Niacin and derivatives Niceritrol • Niacin • Nicofuranose• Aluminium nicotinate• Nicotinyl alcohol • Acipimox CETP inhibitors Anacetrapib† • Torcetrapib§ Combinations Niacin/lovastatin • Niacin/simvastatin • Ezetimibe/simvastatin Other Dextrothyroxine • Probucol • Tiadenol • Benfluorex • Meglutol • Omega-3-triglycerides • Magnesium pyridoxal 5-phosphate glutamate • Policosanol • Ezetimibe • Laropiprant†, Lapaquistat§ †Undergoing clinical trials. ‡Withdrawn from market. §Development terminated.